Cocaine is a tropane alkaloid extracted from the leaves of the coca plant.[3] The name comes from "coca" and the alkaloid suffix "-ine", forming "cocaine". It is thought to be markedly more dangerous than other CNS stimulants, including the entire amphetamine drug class.[4] Regular use has been linked to the development of permanent heart conditions and at high doses it can cause sudden cardiac death.[5]

According to a 2007 United Nations report, cocaine is the second most widely used illicit substance in the world behind cannabis. In terms of user rates, Spain is the country with the highest rate of cocaine usage (3.0% of adults in the previous year).[6] Other countries where the usage rate meets or exceeds 1.5% are the United States (2.8%), England and Wales (2.4%), Canada (2.3%), Italy (2.1%), Bolivia (1.9%), Chile (1.8%), and Scotland (1.5%).[7]

Chemistry

Cocaine is a tropane alkaloid found in the leaves of the coca plant, Erythroxylum coca. It is most commonly consumed as the hydrochloride salt which is typically produced in clandestine laboratories. Cocaine decomposes when heated strongly so the freebase and hydrogen carbonate salts of cocaine, which have much lower boiling points compared to the hydrochloride salt, are typically used when the substance is to be vaporized and are known as cocaine base and crack respectively.

The chemical structure of cocaine consists of three parts; the hydrophilic methyl ester moiety and the lipophilic benzoyl ester moiety, which are located in place of the carboxylic acid and hydroxyl groups of ecgonine respectively. This structure allows for its rapid absorption through nasal membranes and blood-brain barrier.

The presence of the two ester groups makes cocaine relatively unstable in warm, humid environments and cocaine stored in an open container or with a high moisture content will lose apparent potency over time due to hydrolysis to methyl ecgonine or benzoylecgonine.

Cocaine is structurally similar to atropine and scopolamine, which also contain the tropane moiety.

Pharmacology

The most extensively studied effect of cocaine on the central nervous system is the blockade of the dopamine transporter. This substance acts as a reuptake inhibitor and prevents dopamine from being recycled, causing excessive amounts to build up in the synapse, or junction between neurons. The result is an enhanced and prolonged post-synaptic effect of dopaminergic signaling. To a lesser extent, cocaine also exhibits functionally similar effects of reuptake inhibition upon the neurotransmitters of serotonin and noradrenaline.[8] It is this sudden flood of neurotransmitters that causes cocaine’s characteristic high.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWikicontributors. These effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects

Stimulation - Cocaine is reported to be extremely energetic and stimulating in a fashion that is comparatively weaker than methamphetamine, but stronger than that of amphetamine, modafinil, caffeine, and methylphenidate. The particular style of stimulation which cocaine presents can be described as encouraged at low to moderate dosages but forced at higher dosages. This means that at certain dosages, it becomes difficult or impossible to keep still as jaw clenching, involuntarily bodily shakes and vibrations become present, resulting in extreme shaking of the entire body, unsteadiness of the hands, and a general lack of fine motor control. This effect is replaced with mild fatigue and general exhaustion during the offset of the experience.

Abnormal heartbeat - Cocaine consistently raises one's heart rate to abnormally high levels which can be potentially dangerous with prolonged or high dosages.

Tactile hallucination[9] - High doses and/or prolonged usage of certain stimulants like methamphetamine and cocaine can lead to hallucinatory sensations of bugs crawling on the surface of or underneath one’s skin. This is typically referred to as delusional parasitosis or more informally as “coke bugs”.

Teeth grinding - This component can be considered to be less intense when compared with that of MDMA.

Cognitive effects

The cognitive effects of cocaine can be broken down into several components which progressively intensify proportional to dosage. The general head space of cocaine is described by many as one of extreme mental stimulation, increased focus, and powerful euphoria. It contains a large number of typical stimulant cognitive effects. Although negative side effects are usually mild at low to moderate dosages, they become increasingly likely to manifest themselves with higher amounts or extended usage. This particularly holds true during the offset of the experience.
The most prominent of these cognitive effects generally include:

After effects

The effects which occur during the offset of a stimulant experience generally feel negative and uncomfortable in comparison to the effects which occurred during its peak. This is often referred to as a "comedown" and occurs because of neurotransmitter depletion. Its effects commonly include:

Experience reports

Common usage

Cocaine is often adulterated when sold on black markets and this can significantly alter its effects on the body. Even when adulterants are pharmacologically inactive, their combination with the long-term perishability of cocaine due to moisture can lead to vastly differing apparent potencies between dosages of cocaine, and as such, it can be challenging to determine a "typical" recreational dose. Pure cocaine is very potent and generates perceptible local anesthetic effects from 1 mg and perceptible CNS stimulation from 5-7 mg, however in recreational settings much higher doses tend to be used.

Forms

In order for cocaine (in plastic bag at bottom) to be converted to crack, several supplies are needed. Pictured here are baking soda (a commonly used base in making crack) a metal spoon, a tea light, and a cigarette lighter. The spoon is held over the heat source in order to "cook" the cocaine into crack.

Cocaine paste: is a crude extract of the coca leaf which contains 40% to 91% cocaine sulfate along with companion coca alkaloids and varying quantities of benzoic acid, methanol, and kerosene.

Salts: Cocaine is a weakly alkaline compound (an "alkaloid") and can, therefore, combine with acidic compounds to form various salts. The hydrochloride (HCl) salt of cocaine is by far the most commonly encountered, although the sulfate (-SO4) and the nitrate (-NO3) are occasionally seen. Different salts dissolve to a greater or lesser extent in various solvents. The hydrochloride salt is polar in character and quite soluble in water.

Freebase: “Freebase” is the base form of cocaine, as opposed to the salt form. It is practically insoluble in water whereas hydrochloride salt is water soluble. This prevents cocaine in its basic form from being usable for sublingual usage and insufflation. Freebase cocaine can be treated with ethers, isopropyl alcohol, and hydrochloric acid to turn it into the salt form. [12]

"Crack": Crack refers to a lower purity form of freebase cocaine that is usually produced by neutralization of cocaine hydrochloride with a solution of baking soda (sodium bicarbonate, NaHCO3) and water, producing a very hard/brittle, off-white-to-brown colored, amorphous material that contains sodium carbonate, entrapped water, and other by-products as the main impurities. Smoking or vaporizing cocaine and inhaling it into the lungs produces an almost immediate "high" that can be very powerful and addictive. This initial buildup of stimulation is known as a "rush". While the stimulating effects may last for hours, the euphoric sensation is very brief, prompting the user to smoke more immediately.

Coca leaf infusions: Coca herbal infusion (also referred to as coca tea) is used in coca-leaf producing countries as much as any herbal medicinal infusion would be elsewhere in the world. The free and legal commercialization of dried coca leaves under the form of filtration bags to be used as "coca tea" has been actively promoted by the governments of Peru and Bolivia for many years as a drink having medicinal properties. The leaves are also very widely used by native populations for a variety of purposes including the treatment of altitude sickness.

Coca leaf chewing: Chewing the leaves with lime is also common in producing regions, which numbs the mouth and causes mild stimulation.

Toxicity and harm potential

Occasional use of cocaine rarely causes permanent or severe trouble to the body and mind.[14][15] In terms of neurotoxicity (as defined by the damage or death of cells in the brain in response to over-excitation or reactive oxidation caused by drugs), cocaine does not appear to exhibit these effects unlike certain other substances such as methamphetamine. Its extended use or abuse does, however, cause short-term down regulation of neurotransmitters.

The most potentially harmful physical effects of cocaine appear to be not neurological but cardiovascular. Severe cardiac adverse events, particularly sudden cardiac death, become a serious risk at high doses due to cocaine's blocking effect on cardiac sodium channels.[16]
Moreover, long-term cocaine use may result in cocaine-related cardiomyopathy.[17]

Regular cocaine insufflation, the most popular method of ingestion, can have extremely adverse effects on one's nostrils, nose, and nasal cavities. These include a loss of the sense of smell, nosebleeds, difficulty swallowing, hoarseness, or a chronically runny nose.

Lethal dosage

Susceptible individuals have died from as little as 30 mg applied to mucous membranes, whereas addicts may tolerate up to 5 grams daily.[18]

Tolerance and addiction potential

As with other stimulants, the chronic use of cocaine can be considered highly addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal effects may occur if a person suddenly stops their usage. Addiction is a serious risk with heavy recreational cocaine use but is unlikely to arise from typical medical use.

Tolerance to many of the effects of cocaine develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). Cocaine presents cross-tolerance with all dopaminergicstimulants, meaning that after the consumption of cocaine all stimulants will have a reduced effect.

Withdrawal symptoms

After taking cocaine on a regular basis, some users will become addicted. When the drug is discontinued immediately, the user will experience what has come to be known as a "crash" along with a number of other cocaine withdrawal symptoms including paranoia, depression, anxiety, itching, mood swings, irritability, fatigue, insomnia, an intense craving for more cocaine, and, in some cases, nausea and vomiting. Some cocaine users also report having similar symptoms to schizophrenic patients and feel that their mind is scattered or incoherent. Some users also report a feeling of a crawling sensation on the skin also known as "coke bugs".

These symptoms can last for weeks or, in some cases, months. Even after most withdrawal symptoms dissipate most users feel the need to continue using the drug; this feeling can last for years and may peak during times of stress. About 30-40% of cocaine addicts will turn to other substances such as medication and alcohol after giving up cocaine.[citation needed]

Psychosis

Cocaine has a similar potential to induce temporary psychosis[19] with more than half of cocaine abusers reporting at least some psychotic symptoms at some point.[20] Typical symptoms of sufferers include paranoid delusions that they are being followed and that their drug use is being watched accompanied by hallucinations that support the delusional beliefs.[21]Delusional parasitosis with formication ("cocaine bugs") is also a fairly common symptom.[21]

Cocaine-induced psychosis shows sensitization toward the psychotic effects of the drug. This means that psychosis becomes more severe with repeated intermittent use.[22]

Dangerous interactions

Although many psychoactive substances are safe to use on their own, they can quickly become dangerous or even life-threatening when combined with other substances. The following lists some known dangerous combinations, but may not include all of them. A combination that appears to be safe in low doses can still increase the risk of injury or death. Independent research should always be conducted to ensure that a combination of two or more substances is safe to consume. Some interactions listed have been sourced from Tripsit.

Mushrooms - Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences.

LSD - Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences.

DMT - Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences.

Mescaline - The focus and anxiety caused by stimulants is magnified by psychedelics and results in an increased risk of thought loops.

2C-x - The anxiogenic and focusing effects of stimulants increase the chance of unpleasant thought loops. The combination is generally unnecessary because of the stimulating effects of psychedelics. Combination of the stimulating effects may be uncomfortable.

Cannabis - Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences.

Ketamine - No unexpected interactions, though likely to increase blood pressure but not an issue with sensible doses. Moving around on high doses of this combination may be ill advised due to risk of physical injury.

MXE - Stimulants taken with MXE can lead to hypermanic states much more easily, especially if sleep is avoided.

Amphetamines - This combination of stimulants will increase strain on the heart. It is not generally worth it as Cocaine has a mild blocking effect on dopamine releasers like amphetamine.

MDMA - Cocaine blocks some of the desirable effects of MDMA while increasing the risk of heart attack.

GHB - Stimulants increase respiration rate allowing a higher dose of sedatives. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest. Likewise the G can wear off and leave a dangerous concentration of Cocaine behind.

GBL - Stimulants increase respiration rate allowing a higher dose of sedatives. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest. Likewise the G can wear off and leave a dangerous concentration of Cocaine behind.

DOx - The combined stimulating effects of the two can lead to an uncomfortable body-load, while the focusing effects of Cocaine can easily lead to thought loops. Coming down from Cocaine while the DOx is still active can be quite anxiogenic.

25x-NBOMe - Cocaine and NBOMes both provide considerable stimulation. When combined they can result in severe vasoconstriction, tachycardia, hypertension, and in extreme cases heart failure.

2C-T-x - Cocaine and 2C-T-x both provide considerable stimulation. When combined they can result in severe vasoconstriction, tachycardia, hypertension, and in extreme cases heart failure.

5-MeO-xxT - The anxiogenic and focusing effects of stimulants increase the chance of unpleasant thought loops. The combination is generally unnecessary because of the stimulating effects of psychedelics.

DXM - Both substances raise heart rate, in extreme cases, panic attacks caused by these drugs have led to more serious heart issues.

PCP - This combination can easily lead to hypermanic states.

Alcohol - Drinking while using stimulants is risky because the sedative effects of alcohol are reduced. These are what the body uses to gauge “drunkenness”. This typically leads to excessive drinking with greatly reduced inhibitions, high risk of liver damage and increased dehydration. They will also allow you to drink past a point where you might normally pass out, increasing the risk. If you do decide to do this then you should set a limit of how much you will drink each hour and stick to it, bearing in mind that you will feel alcohol less. Cocaine is potentiated somewhat by alcohol because of the formation of cocaethylene.

ΑMT

Opioids - Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.

Tramadol - Tramadol and stimulants both increase the risk of seizures.

Legal status

Austria: Cocaine is illegal to possess, produce and sell under the SMG (Suchtmittelgesetz Österreich)..[citation needed]

Bolivia: Limited cultivation of coca is legal in Bolivia, where chewing the leaves and drinking coca tea are considered cultural practices, in particular, in the mountainous regions. Processed cocaine is illegal.[citation needed]

Brazil: Cocaine is often sold openly in stores, but it still remains illegal. In most cases, the stores will pay off the police to look the other way.[citation needed]

Canada: Cocaine is a Schedule I drug under the Controlled Drugs and Substances Act of Canada.[23]

Colombia: In 1994, possession of 1 gram of cocaine was legalized for personal use.[24][25] Sale remains illegal, but personal production or gifts of cocaine are permitted.[citation needed]

Germany: Possession of cocaine without a medical prescription is illegal. Small amounts for self-consumption may go unpunished for the first time or non-regular offenders. This also varies by state. Usually, revocation of a driving license will follow up the confiscation of any drug except marijuana, since drug users are considered a risk to road traffic.[citation needed]

Hong Kong: Use and possession of cocaine is illegal unless a license was issued by the Department of Health.[citation needed]

India: Use and possession of cocaine is illegal with a mandatory 10-year sentence.[citation needed]

Lithuania: Cocaine is a schedule I substance. Possession, production, and trade are not allowed.[26]

Mexico: As of August 25, 2009, the Mexican legislature officially legalized small doses of cocaine, heroin, marijuana, crystal meth, and ecstasy for personal use. No action will be taken for those carrying up to half a gram of cocaine.[27][28][29][30][31]

Netherlands: Cocaine is considered an illegal hard drug. Possession, production, and trade are not allowed as stated in the Opium Law of 1928. Although technically illegal, possession of less than half a gram usually goes unpunished.[32][33]

New Zealand: Cocaine is a Class A drug. The coca leaf and preparations of cocaine containing no more than 0.1% cocaine base, in such a way that the cocaine cannot be recovered, are both classified as Class C.[citation needed]

Peru: Cultivation of coca plants is legal and coca leaves are sold openly on markets. Similarly to Bolivia, chewing leaves and drinking coca tea belong to cultural practices. Possession of up to 2 grams of cocaine or up to 5 grams of cocaine basic paste is legal for personal use in Peru per Article 299 of Peruvian Penal Code.[34] However, the reality of how police treats it might be very different.[35] An important part of Article 299 is that person may not possess two or more kinds of drugs at the same time -- this would make it a criminal offense.

Portugal: Personal use of cocaine is decriminalized. Drug abuse is dealt with by administrative and medical intervention. Trafficking is illegal.[36]

Saudi Arabia: Use and possession of cocaine is punishable by death.[citation needed]

Singapore: Possession of more than 30 grams of cocaine results in a mandatory death sentence, but can be issued by the Department of Health.[citation needed]

South Africa: It is a crime to have cocaine in your possession.[citation needed]

Switzerland: Personal use of cocaine is sentenced to a fine. Trafficking is sentenced to jail.[citation needed]

United Kingdom: Cocaine is a Class A drug, controlled by the Misuse of Drugs Act 1971. However, medical use by doctors for controlling pain is permitted.[citation needed]

United States: Cocaine is classified as a Schedule II Narcotic under the Controlled Substances Act of the United States.[37]